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S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nat Commun, 2024, 15(1):987
Acta Biomater, 2024, S1742-7061(24)00036-9
Cell Death Dis, 2024, 15(1):31
S1574 Doramapimod (BIRB 796) Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.
Aging Cell, 2024, e14093.
Cell Rep, 2023, 42(6):112547
Int J Mol Sci, 2023, 10.3390/ijms242216538
S1950 Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Clin Respir J, 2024, 18(1):e13731
Cell Death Dis, 2023, 14(7):469
Cell Death Dis, 2023, 14(7):469
S4901 JNK-IN-8 JNK-IN-8 (JNK Inhibitor XVI) is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line.
Mil Med Res, 2023, 10(1):56
J Exp Med, 2023, 220(9)e20230054
Cell Rep, 2023, 42(6):112547
S7409 Anisomycin Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis.
Theranostics, 2024, 14(4):1561-1582
Acta Biomater, 2024, S1742-7061(24)00036-9
Int J Biol Sci, 2024, 20(2):784-800
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S5958 Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Adv Healthc Mater, 2024, e2303785.
Kidney Int, 2023, 103(5):917-929
Free Radic Biol Med, 2023, 206:1-12
S7508 JNK Inhibitor IX JNK inhibitor IX (TCS JNK 5a) is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively.
Cell Mol Immunol, 2023, 20(8):908-923
Nat Commun, 2023, 14(1):3364
Nat Commun, 2020, 11(1):258
S8490 Tanzisertib(CC-930) Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.
Signal Transduct Target Ther, 2023, 8(1):94
Viruses, 2023, 15(5)1112
Elife, 2022, 11e80953
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Cell Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Cell Cycle, 2022, 1-14
S7794 JNK Inhibitor VIII JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.
Cell Death Discov, 2022, 8(1):113
Molecules, 2021, 26(8)2141
PLoS Pathog, 2018, 14(11):e1007418
S8867 Bentamapimod (AS602801) Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively.
Front Oncol, 2022, 12:1006131
Nat Biomed Eng, 2018, 2(8):578-588
S3292 Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Pharmacol, 2021, 12:656697
S8201 BI-78D3 BI-78D3 is a competitive JNK inhibitor with IC50 of 280nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K.
Neoplasia, 2021, 23(7):718-730
Cell Discov, 2019, 5:2
E1391New SP 600125, negative control SP 600125, negative control (JNK inhibitor II, negative control) is a methylated analog of SP 600125 and inhibits JNK2 and JNK3 with IC50 of 18 µM and 24 µM, respectively.
Cell Death Dis, 2023, 14(8):537
S7637 DTP3 DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
MedComm (2020), 2023, 4(3):e269
S6730 CC-401 Hydrochloride CC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases.
Insect Biochem Mol Biol, 2016, 73:55-61
S3811 Ginsenoside Re Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S9114 Polyphyllin I Polyphyllin I, a small molecular monomer extracted from Rhizoma of Paris polyphyllin, is used in the treatment of infectious disease and cancer. Polyphyllin I inhibits proliferation and induces apoptotic cell death in U251 cells. Polyphyllin I is an activator of the JNK signaling pathway with a potential anti-glioma effect.
Oxid Med Cell Longev, 2022, 2022:4031008
S6740 DB07268 DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK.
S3940 3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies.
S4643 KB-R7943 mesylate KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.
E2653 JNK-IN-7 JNK-IN-7 is a strong  JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, which inhibits phosphorylation of c-Jun, direct substrate of JNK kinase.
S3242 Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S4884 Trans-Zeatin Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently.
S9614New CC-90001 CC-90001 is an orally administered inhibitor of c-Jun N-terminal kinase (JNK) with bias for JNK1 over JNK2. It exhibits antifibrotic efficacy and can be used for the research of idiopathic pulmonary fibrosis.
S9698 Ezatiostat Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis.
S0781 IQ 3 IQ 3 is a specific c-Jun N-terminal kinase (JNK) inhibitor with Kd of 66 nM, 240 nM and 290 nM for JNK3, JNK1 and JNK2, respectively. IQ 3 inhibits LPS-induced NF-κB/AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM. IQ 3 also inhibits TNF-α and IL-6 production in vitro.
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
E2252 SU3327 SU3327 is a potent, selective and substrate-competitive c-Jun N-terminal kinase (JNK) inhibitor with an IC50 of 0.7 μM.
E1656New AS601245 AS601245 is an orally active, selective, ATP-competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50 of 150, 220, and 70 nM for three JNK human isoforms hJNK1, hJNK2, and hJNK3, respectively.
E0072 Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S0844 NDMC101 NDMC101 inhibits osteoclastogenesis which also ameliorates paw swelling and inflammatory bone destruction, associating with the inhibition of such transcription factors as NF-κB and NFATc1 as well as multiple protein kinases, including p38, ERK, and JNK.
S9075 Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
E2682 RPI-1 RPI-1 inhibits proliferation of human papillary thyroid carcinoma cell line TPC-1 by inducing accumulation of cells at the G2 cell cycle phase, abolishes Ret/Ptc1 tyrosine phosphorylation along with its binding to Shc and phospholipase Cg, also abolishes the activation of JNK2 and AKT.
S4460 IMM-H007 IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux.
S6347 5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.
S6711 IQ-1S IQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively.
S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nat Commun, 2024, 15(1):987
Acta Biomater, 2024, S1742-7061(24)00036-9
Cell Death Dis, 2024, 15(1):31
S1574 Doramapimod (BIRB 796) Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.
Aging Cell, 2024, e14093.
Cell Rep, 2023, 42(6):112547
Int J Mol Sci, 2023, 10.3390/ijms242216538
S4901 JNK-IN-8 JNK-IN-8 (JNK Inhibitor XVI) is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line.
Mil Med Res, 2023, 10(1):56
J Exp Med, 2023, 220(9)e20230054
Cell Rep, 2023, 42(6):112547
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S7508 JNK Inhibitor IX JNK inhibitor IX (TCS JNK 5a) is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively.
Cell Mol Immunol, 2023, 20(8):908-923
Nat Commun, 2023, 14(1):3364
Nat Commun, 2020, 11(1):258
S8490 Tanzisertib(CC-930) Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.
Signal Transduct Target Ther, 2023, 8(1):94
Viruses, 2023, 15(5)1112
Elife, 2022, 11e80953
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Cell Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Cell Cycle, 2022, 1-14
S7794 JNK Inhibitor VIII JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.
Cell Death Discov, 2022, 8(1):113
Molecules, 2021, 26(8)2141
PLoS Pathog, 2018, 14(11):e1007418
S8867 Bentamapimod (AS602801) Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively.
Front Oncol, 2022, 12:1006131
Nat Biomed Eng, 2018, 2(8):578-588
S3292 Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Pharmacol, 2021, 12:656697
S8201 BI-78D3 BI-78D3 is a competitive JNK inhibitor with IC50 of 280nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K.
Neoplasia, 2021, 23(7):718-730
Cell Discov, 2019, 5:2
E1391New SP 600125, negative control SP 600125, negative control (JNK inhibitor II, negative control) is a methylated analog of SP 600125 and inhibits JNK2 and JNK3 with IC50 of 18 µM and 24 µM, respectively.
Cell Death Dis, 2023, 14(8):537
S6730 CC-401 Hydrochloride CC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases.
Insect Biochem Mol Biol, 2016, 73:55-61
S3811 Ginsenoside Re Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S6740 DB07268 DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK.
E2653 JNK-IN-7 JNK-IN-7 is a strong  JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, which inhibits phosphorylation of c-Jun, direct substrate of JNK kinase.
S3242 Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S4884 Trans-Zeatin Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently.
S9614New CC-90001 CC-90001 is an orally administered inhibitor of c-Jun N-terminal kinase (JNK) with bias for JNK1 over JNK2. It exhibits antifibrotic efficacy and can be used for the research of idiopathic pulmonary fibrosis.
S0781 IQ 3 IQ 3 is a specific c-Jun N-terminal kinase (JNK) inhibitor with Kd of 66 nM, 240 nM and 290 nM for JNK3, JNK1 and JNK2, respectively. IQ 3 inhibits LPS-induced NF-κB/AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM. IQ 3 also inhibits TNF-α and IL-6 production in vitro.
E2252 SU3327 SU3327 is a potent, selective and substrate-competitive c-Jun N-terminal kinase (JNK) inhibitor with an IC50 of 0.7 μM.
E1656New AS601245 AS601245 is an orally active, selective, ATP-competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50 of 150, 220, and 70 nM for three JNK human isoforms hJNK1, hJNK2, and hJNK3, respectively.
E0072 Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S9075 Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
E2682 RPI-1 RPI-1 inhibits proliferation of human papillary thyroid carcinoma cell line TPC-1 by inducing accumulation of cells at the G2 cell cycle phase, abolishes Ret/Ptc1 tyrosine phosphorylation along with its binding to Shc and phospholipase Cg, also abolishes the activation of JNK2 and AKT.
S4460 IMM-H007 IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux.
S6347 5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.
S6711 IQ-1S IQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively.
S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S1950 Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Clin Respir J, 2024, 18(1):e13731
Cell Death Dis, 2023, 14(7):469
Cell Death Dis, 2023, 14(7):469
S7409 Anisomycin Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis.
Theranostics, 2024, 14(4):1561-1582
Acta Biomater, 2024, S1742-7061(24)00036-9
Int J Biol Sci, 2024, 20(2):784-800
S5958 Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Adv Healthc Mater, 2024, e2303785.
Kidney Int, 2023, 103(5):917-929
Free Radic Biol Med, 2023, 206:1-12
S7637 DTP3 DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
MedComm (2020), 2023, 4(3):e269
S9114 Polyphyllin I Polyphyllin I, a small molecular monomer extracted from Rhizoma of Paris polyphyllin, is used in the treatment of infectious disease and cancer. Polyphyllin I inhibits proliferation and induces apoptotic cell death in U251 cells. Polyphyllin I is an activator of the JNK signaling pathway with a potential anti-glioma effect.
Oxid Med Cell Longev, 2022, 2022:4031008
S3940 3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies.
S4643 KB-R7943 mesylate KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.
S9698 Ezatiostat Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis.
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
E1391New SP 600125, negative control SP 600125, negative control (JNK inhibitor II, negative control) is a methylated analog of SP 600125 and inhibits JNK2 and JNK3 with IC50 of 18 µM and 24 µM, respectively.
Cell Death Dis, 2023, 14(8):537
S9614New CC-90001 CC-90001 is an orally administered inhibitor of c-Jun N-terminal kinase (JNK) with bias for JNK1 over JNK2. It exhibits antifibrotic efficacy and can be used for the research of idiopathic pulmonary fibrosis.
E1656New AS601245 AS601245 is an orally active, selective, ATP-competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50 of 150, 220, and 70 nM for three JNK human isoforms hJNK1, hJNK2, and hJNK3, respectively.

JNK阻害剤の選択性比較

Tags: JNK inhibitor|JNK agonist|JNK activator|JNK inducer|JNK antagonist|JNK signaling pathway|JNK assay kit